CAS: 1070-11-7; (2S,2'S)-2,2'-(Ethane-1,2-Diylbis(Azanediyl))Bis(Butan-1-Ol) Dihydrochloride

该化合物是一种主要用于治疗结核病的抗菌菌剂,其关键优点包括水溶性高,确保生物利用率一致,在标准储存条件下保持稳定;二氯化二苯胺配方通过改进吸收和治疗应用中的分布,提高了其功效;作为细菌制剂,它具体针对的是抑制异丙醇转移酶的分子细胞壁合成;二氯化乙胺醇通常与其他抗菌药物结合,以防止抗药性发展;其有详细记载的药用动力学特征和既定的安全性使二氯化二苯乙胺在一线结核病疗法中成为可靠的成分;建议适当处理和储存以保持其化学完整性.

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    专利信息


    专利号:US-3944619-A
    优先权日:1976-02-20
    标 题 :Synthesis of d-2-amino-1-butanol
    发明人:SINGH BALWANT
    权利人:AMERICAN CYANAMID CO
    摘要:D-2-Amino-1-butanol, for the synthesis of ethambutol hydrochloride, d,d'-2,2'-(ethylenediimino)di-1-butanol dihydrochloride, is produced in high purity and good yields by the reaction of butene-1, a nitrile, preferably an excess of acetonitrile, and chlorine to form N-[1-(chloromethyl)propyl]acetimidoyl chloride which is hydrolyzed to dl-2-amino-1-butanol, which can be isolated as the hydrochloride, or free base, or a mixture, resolved with L(+)- tartaric acid and the d-2-amino-1-butanol reacted with ethylene dichloride and then hydrochloric acid to form ethambutol hydrochloride. A minimum of by-products which are conveniently split out permits the economical synthesis of a pharmaceutical grade product.

    专利号:US-8557979-B2
    优先权日:2004-06-10
    标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
    发明人:CHOI WOO-BAEG; KOWALIK EWA
    权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    专利号:US-10933051-B2
    优先权日:2017-06-09
    标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
    发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
    权利人:FOB SYNTHESIS INC
    摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

    专利号:US-9693999-B2
    优先权日:2011-01-26
    标题:Small molecule RNase inhibitors and methods of use
    发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
    权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
    摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

    专利号:US-9937151-B2
    优先权日:2010-06-18
    标题 :Carbapenem antibacterials with gram-negative activity
    发明人:CHOI WOO-BAEG; GRUSZECKA-KOWALIK EWA; JOO HYUNG-YEUL; LIU SHUANGPEI; MAO SHULI; LI YONGFENG; KIM DEOG-IL
    权利人:FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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    主要参考文献


    1: El-Ridy MS, Yehia SA, Kassem MA, Mostafa DM, Nasr EA, Asfour MH. Niosomal encapsulation of ethambutol hydrochloride for increasing its efficacy and safety. Drug Deliv. 2015 Jan;22(1):21-36. doi: 10.3109/10717544.2013.868556. Epub 2013 Dec 20. doi: 10.5740/jaoacint.14-237. doi: 10.5588/ijtld.13.0190. doi: 10.1016/j.rmr.2014.03.011. Epub 2014 Apr 29. French. Chinese. doi: 10.1016/j.toxlet.2014.06.006. Epub 2014 Jun 5. doi: 10.1016/j.ijpharm.2014.12.053. Epub 2014 Dec 26. doi: 10.4088/JCP.14m09403. doi: 10.3109/08958378.2014.975875. doi: 10.1186/s12879-015-0862-7.
    15: He L, Wang X, Cui P, Jin J, Chen J, Zhang W, Zhang Y. ubiA (Rv3806c) encoding DPPR synthase involved in cell wall synthesis is associated with ethambutol resistance in Mycobacterium tuberculosis. Tuberculosis (Edinb). 2015 Mar;95(2):149-54. doi: 10.1016/j.tube.2014.12.002. Epub 2014 Dec 13. doi: 10.1093/jac/dkt448. Epub 2013 Nov 11. doi: 10.1111/jvp.12119. Epub 2014 Mar 29. doi: 10.1097/INF.0000000000000589.

    合成参考文献


    摘要:American Review of Respiratory Disease., 83(891), 1961 []
    摘要:Oyo Yakuri. Pharmacometrics., 2(70), 1968
    参考文献:10.1016/j.bmcl.2014.05.026
    摘要:Voynikov Y, Valcheva V, Momekov G, Peikov P, Stavrakov G. Theophylline-7-acetic acid derivatives with amino acids as anti-tuberculosis agents. Bioorganic & Medicinal Chemistry Letters. 2014 Jul;24(14):3043–5. doi: 10.1016/j.bmcl.2014.05.026.
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